2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. FXR

FXR

FXR; NR1H4

FXR

Related Products

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Farnesoid X receptor (FXR) is a ligand-activated transcription factor belonging to the nuclear receptor superfamily. FXR regulates the expression of various genes by binding to DNA either as a monomer or a heterodimer with the common partner for NRs, retinoid x receptor (RXR), to FXR response elements. Two known FXR genes exist, the FXRα and FXRβ.

FXR is mainly expressed in liver and small intestine, where it plays an important role in bile acid, lipid, and glucose metabolism. FXR affects several metabolic pathways through its specific target genes, regulating bile acid (BA) synthesis and homeostasis, glucose and lipid metabolism, also exhibiting a crucial role in intestinal bacterial growth and liver regeneration.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-168327
    LH10
    		Agonist
    LH10 is a fexaramine-based agonist for FXR with an EC50 of 0.14 μM. LH10 exhibits liver protection efficacy, ameliorates the alpha naphthylisothiocyanate (ANIT)-induced cholestasis, APAP (HY-66005)-induced acute liver injury and non-alcoholic steatohepatitis (NASH) in mouse models.
    LH10
  • HY-159845
    Lecufexor
    		Agonist 99.27%
    Lecufexor is a farnesoid X receptor (FXR) agonist.
    Lecufexor
  • HY-135399S
    Tauro-obeticholic acid-d5 sodium
    		Agonist
    Tauro-obeticholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid sodium (HY-135399A). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
    Tauro-obeticholic acid-d<sub>5</sub> sodium
  • HY-N1423AR
    Glycocholic acid sodium (Standard)
    		Inhibitor
    Glycocholic acid (sodium) (Standard) is the analytical standard of Glycocholic acid sodium (HY-N1423A). This product is intended for research and analytical applications. Glycocholic acid sodium is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid sodium (Standard)
  • HY-N4294R
    Arjungenin (Standard)
    		Agonist
    Arjungenin (Standard) is the analytical standard of Arjungenin. This product is intended for research and analytical applications. Arjungenin, a pentacyclic triterpenoid compound, is a FXR agonist. Arjungenin can improve insulin sensitivity by regulating the function of fat cells. Arjungenin exhibits moderate free radical scavenging activity. Arjungenin has growth inhibitory activity against the insect Spilarctia obliqua. Arjungenin has significant antiviral activity against a series of viruses such as chikungunya Virus (CHIKV).
    Arjungenin (Standard)
  • HY-135399S2
    Tauro-obeticholic acid-d4
    Tauro-obeticholic acid-d4 is the deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
    Tauro-obeticholic acid-d<sub>4</sub>
  • HY-183309
    FXR/HSD17B13-modulator-2
    		Agonist
    FXR/HSD17B13-modulator-2 is a dual FXR activator and HSD17B13 inhibitor with human FXR EC50 of 128 nM, human HSD17B13 IC50 of 0.18 μM, high selectivity over related nuclear receptors and HSD17B isoforms, and oral effectiveness.FXR/HSD17B13-modulator-2 alleviates fatty liver, regulates lipid metabolism, reduces inflammation, and attenuates hepatic fibrosis.FXR/HSD17B13-modulator-2 is the first non-carboxylic acid dual FXR/HSD17B13 modulator.FXR/HSD17B13-modulator-2 can be used for the research of metabolic dysfunction-associated steatohepatitis.
    FXR/HSD17B13-modulator-2
  • HY-110066R
    (Z)-Guggulsterone (Standard)
    		Antagonist
    (Z)-Guggulsterone (Standard) is the analytical standard of (Z)-Guggulsterone. This product is intended for research and analytical applications. (Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis. (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection.
    (Z)-Guggulsterone (Standard)
  • HY-76847S1
    Chenodeoxycholic Acid-d9
    		Activator
    Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d<sub>9</sub>
  • HY-117601
    11-Deoxyalisol B
    11-Deoxyalisol B, a triterpene, shows the potent inhibitory activity on Lipopolysaccharide (LPS)-induced nitric oxide (NO) production.
    11-Deoxyalisol B
  • HY-W654353
    Tauro-α-muricholic acid-d4-1 sodium
    		Antagonist
    Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal.
    Tauro-α-muricholic acid-d<sub>4</sub>-1 sodium
  • HY-101274A
    (3α,5β,6β,7α)-BAR501
    		98.0%
    (3α, 5β, 6β, 7α)-BAR501 (BAR504-6b) is a compound having cholane scaffolds of formula. (3α, 5β, 6β, 7α)-BAR501 can be used for the research of FXR and TGR5/GPBAR1 mediated diseases.
    (3α,5β,6β,7α)-BAR501
  • HY-B1734
    16-Dehydropregnenolone acetate
    		Antagonist
    16-Dehydropregnenolone acetate (16-DPA), a sterols compound, is an orally active 17α-hydroxylase and 5α-reductase inhibitor. 16-Dehydropregnenolone is also a potent bile acid receptor (BAR)/farnesoid X receptor (FXR) antagonist. 16-Dehydropregnenolone hypolipidemic and anticancer effects. 16-Dehydropregnenolone acetate (16-DPA) is the drug intermediate that can be used for synthesis of Dexamethasone (HY-14648) and related other steroidal pharmacophores.
    16-Dehydropregnenolone acetate
  • HY-N0805R
    Alisol B 23-acetate (Standard)
    		Activator
    Alisol B 23-acetate (Standard) is the analytical standard of Alisol B 23-acetate (HY-N0805). This product is intended for research and analytical applications. Alisol B 23-acetate is an orally active prototerpane-type triterpenoid. Alisol B 23-acetate can be isolated from Alisma orientalis. Alisol B 23-acetate induces Apoptosis, promotes ROS generation, downregulates CDK4/6, MMP-2/9, upregulates cleaved PARP, activates FXR and inhibits Syk. Alisol B 23-acetate has anti-inflammatory and hepatoprotective activities. Alisol B 23-acetate protects the kidney from ischemia-reperfusion injury. Alisol B 23-acetate has anticancer activity against ovarian cancer, colon cancer, lung cancer, and gastric cancer. Alisol B 23-acetate can be used in the study of atherosclerosis and allergic asthma.
    Alisol B 23-acetate (Standard)
  • HY-W020788R
    Benoxacor (Standard)
    		Activator
    Benoxacor (Standard) is the analytical standard of Benoxacor. This product is intended for research and analytical applications. Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity.
    Benoxacor (Standard)
  • HY-135103S
    Tauro-β-muricholic acid-d4 sodium
    		Antagonist
    Tauro-β-muricholic acid-d4 (sodium) is the deuterium labeled Tauro-β-muricholic acid sodium. Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
    Tauro-β-muricholic acid-d<sub>4</sub> sodium
  • HY-117918
    ST-1892
    		Agonist
    ST-1892 (compound 14) is a highly potent FXR agonist (EC50=7.2 nM) that can be used to study diseases or disorders caused by metabolic inflammation.
    ST-1892
  • HY-113567
    GSK2324
    		Agonist
    GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively.
    GSK2324
  • HY-107738R
    Guggulsterone (Standard)
    		Antagonist
    Guggulsterone (Standard) is the analytical standard of Guggulsterone (HY-107738). This product is intended for research and analytical applications. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.
    Guggulsterone (Standard)
  • HY-133969
    5β-Cholane
    		Activator
    5β-Cholane is a farnesoid X receptor (FXR) activator. 5β-Cholane can be used for the research of cholesterol and lipid-related diseases.
    5β-Cholane
Cat. No. Product Name / Synonyms Application Reactivity